Table 3.
Pharmacokinetics of Diclofenac and Hydroxypropyl‐β‐Cyclodextrin (HPβCD) by Hepatic Function, Following Administration of Intravenous HPβCD‐Diclofenac
| Parametera | Mild Hepatic Impairmentb (n = 8) | Healthy Subjects (n = 7) | P |
|---|---|---|---|
| Diclofenac | |||
| Cmax (ng/mL) | 5648 ± 709 | 5884 ± 897 | .61 |
| AUC∞ (ng·h/mL) | 1663 ± 179 | 1640 ± 335 | .76 |
| t½ (h) | 1.97 ± 0.67 | 1.92 ± 0.28 | .97 |
| CL (mL/min) | 353 ± 40.7 | 367 ±74.7 | .76 |
| Vz (L) | 60.1 ± 21.5 | 59.9 ± 9.4 | .81 |
| Tmax (h) | 0.083 | 0.083 | – |
| AUC(0‐t) (ng·h/mL) | 1641 ± 179 | 1618 ± 333 | – |
| HPβCD | |||
| Cmax (ng/mL) | 44 813 ± 14 985 | 40 917 ± 4975 | .74 |
| AUC∞ (ng·h/mL) | 56 802 ±17 412 | 53 651 ± 11 321 | .82 |
| t½ (h) | 2.28 ± 0.60 | 2.28 ± 0.42 | .91 |
| CL (mL/min) | 107 ± 33.8 | 107 ± 21.2 | .82 |
| Vz (L) | 20.0 ± 4.19 | 20.6 ± 2.45 | .62 |
| Tmax (h) | 0.083 | 0.083 | – |
| AUC0–t (ng·h/mL) | 55 946 ± 17 233 | 52 982 ± 11 267 | – |
Cmax, maximum observed plasma concentration; Tmax, time at which Cmax was observed; AUC0–t, AUC up to the last quantifiable concentration; AUC∞, AUC from time zero to infinity; t½, apparent elimination half‐life; Vz, volume of distribution; CL, clearance.
a
All parameters are presented as arithmetic mean ± standard deviation (SD), except for Tmax, for which the median is reported.
b
Child‐Pugh Classification A score 5–6; serum bilirubin ≤ 2.5 mg/dL.